Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.

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Nyandege A, Kolanos R, Roth BL, Glennon RA

Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1691-4. Epub 2007 Jan 4.

PubMed ID

17239595 [ View in PubMed

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Abstract

N(1)-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT(6) receptors. Replacement of the aryl moiety with similarly hydrophobic alkyl substituents results in decreased affinity, as does replacement of a benzenesulfonyl moiety with a benzyl group. Current findings indicate that an aryl (or substituted aryl) sulfonyl (rather than alkylsulfonyl or benzyl) moiety is optimal for high-affinity binding, and further suggest that the N(1)-benzenesulfonyl- and their corresponding N(1)-benzyltryptamine counterparts bind in a different fashion.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dimethyltryptamine	5-hydroxytryptamine receptor 6	Protein	Humans	Yes	Not Available	Details